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Journal of Asian Natural Products Research

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https://www.readbyqxmd.com/read/30187782/comparative-analysis-of-stimulation-and-binding-characteristics-of-adenosine-analogs-to-amp-activated-protein-kinase
#1
Feng Gao, Yue-Jiao Qian, Fei-Hu Chen, Hai-Bo Zhu
To compare the stimulation and binding characteristics of adenosine analogs including AMP, IMM-H007, and M1, to AMPK, and to explore the potential mechanism underlying the regulation effect of adenosine analogs on AMPK activity, [γ-32 P]ATP assay, circular dichroism experiments and molecular docking test were performed. We found that the interactions with Thr86, Thr88, and His150 in site 1 are probably the reason why the affinities of IMM-H007, M1, and adenosine are comparable but their allosteric activation on AMPK varies greatly, partly interpreting the mechanism of AMPK activity regulated by adenosine analogs...
September 6, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/30130142/pharmacokinetics-of-costunolide-and-dehydrocostuslactone-after-oral-administration-of-radix-aucklandiae-extract-in-normal-and-gastric-ulcer-rats
#2
Shu Dong, Li-Yan Ma, Yue-Tao Liu, Meng Yu, Hong-Mei Jia, Hong-Wu Zhang, Chang-Yuan Yu, Zhong-Mei Zou
Costunolide and dehydrocostuslactone are the main active ingredients of Radix Aucklandiae (RA). An accurate and sensitive LC-MS/MS method was established to simultaneously determine contents of costunolide and dehydrocostuslactone in plasma. There were significant differences in pharmacokinetic parameters (AUC0-t , Cmax,1 , Cmax,2 , Tmax,1 , Vd, and CL) of costunolide and dehydrocostuslactone between RA group and costunolide group or dehydrocostuslactone group. The relative bioavailability of costunolide or dehydrocostuslactone of RA extract was improved...
August 21, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/30129376/three-new-%C3%AE-pyrone-derivatives-from-the-plant-endophytic-fungus-penicillium-ochrochloronthe-and-their-antibacterial-antifungal-and-cytotoxic-activities
#3
Ting Zhao, Lu-Lin Xu, Yan Zhang, Zheng-Hong Lin, Tao Xia, Deng-Feng Yang, Ye-Miao Chen, Xiao-Long Yang
Three new 3,4,6-trisubstituted α-pyrone derivatives, namely 6-(2'R-hydroxy-3'E,5'E-diene-1'-heptyl)-4-hydroxy-3-methyl-2H-pyran-2-one (1), 6-(2'S-hydroxy-5'E-ene-1'-heptyl)-4-hydroxy-3-methyl-2H-pyran-2-one (2), and 6-(2'S-hydroxy-1'-heptyl)-4 -hydroxy-3-methyl-2H-pyran-2-one (3), together with one known compound trichodermic acid (4), were isolated from the solid-substrate fermentation culture of Penicillium ochrochloronthe associated the roots of Taxus media. Compounds 1-4 displayed the antimicrobial activity selectively against tested fungal and bacterial strains with minimum inhibitory concentration (MIC) values ranging from 12...
August 21, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/30129374/six-new-diterpenoids-from-croton-laevigatus
#4
Mo-Nan Liu, Meng-Meng Zhang, Jing-Ya Li, Jia Li, Yao-Yue Fan, Jian-Min Yue
Six new ent-labdane-type diterpeniods (1‒6), along with one known compound, were identified from the twigs and leaves of Croton laevigatus. Their structures were elucidated on the basis of extensive spectroscopic interpretation. Compounds 2 and 7 showed inhibitory activity against protein tyrosine phosphatase 1B (PTP1B) with IC50 values of 4.11 and 8.33 μg/ml, respectively.
August 21, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/30047298/fungi-outstanding-source-of-novel-chemical-scaffolds
#5
Zhen Liu, Jing-Yi Zhao, Sen-Feng Sun, Yong Li, Yun-Bao Liu
A large number of remarkable studies on the secondary metabolites of fungi have been conducted in recent years. This review gives an overview of one hundred and sixty-seven molecules with novel skeletons and their bioactivities that have been reported in seventy-nine articles published from 2013 to 2017. Our statistical data showed that endophytic fungi and marine-derived fungi are the major sources of novel bioactive secondary metabolites.
July 26, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/30047293/sesquiterpenoids-with-cytotoxicity-from-heartwood-of-dalbergia-odorifera
#6
Hui Meng, De-Li Chen, Yun Yang, Yang-Yang Liu, Jian-He Wei
Two new sesquiterpenoids, named dalodorin A (1) and dalodorin B (2), together with four known sesquiterpenoids, were isolated from the heartwood of Dalbergia odorifera. Their structures were elucidated on the basis of spectroscopic analysis including 1D and 2D NMR techniques and HR-ESI-MS. Evaluation of the isolated compounds for cytotoxicity against two human cancer cell lines (Hela and HepG-2) showed moderate activities (25.22-60.45 μM).
July 26, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/30014711/new-steroidal-glycosides-from-the-fibrous-roots-of-ophiopogon-japonicus
#7
Chang-Ling Duan, Yu-Juan Li, Feng-Yun Wang, Lan Miao, Xu-Dong Tang
Two new steroidal glycosides (named fibrophiopogonins A, B), along with one known glycoside, were isolated from the fibrous roots of Ophiopogon japonicus (Liliaceae). Comprehensive spectroscopic analysis, including 2D NMR spectroscopy, and the results of acid hydrolysis allowed the chemical structure of the compounds to be assigned as 26-[(O-β-D-glucopyranosyl-(1 → 6)-D-glucopyranosyl)]-barogenin- 3-O-[α-L-rhamnopyranosyl-(1→2)]-β-D-glucopyranoside and (25R)-26-[(O- β-D-glucopyranosyl-(1→6)-β-D-glucopyranosyl)]- 3β,22α,26- trihydroxyfurost- 5-ene-3-O-[α-L-rhamnopyranosyl-(1→2)]-β-D-glucopyranoside...
July 17, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/30014709/chemical-constituents-from-the-culture-of-the-fungus-hericium-alpestre
#8
Lu-Ning Li, Lei Wang, Xiu-Li Guo
Two new compounds herialpins A-B (1-2), along with eleven known compounds, were isolated from the culture of fungus Hericium alpestre. The structures were elucidated by 1D and 2D NMR data, ESI-MS and X-ray crystallographic analysis. Compounds 1-2 were assayed for their cytotoxicity against three tumor cell lines compared with the known compound 3. Compounds 1 and 2 were found with modest activity, while compound 3 exhibits stronger selective inhibitory activity against A549 and HT-29 cells with IC50 values of 15...
July 17, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/30010416/transcriptome-analysis-of-three-cultivars-of-poria-cocos-reveals-genes-related-to-the-biosynthesis-of-polysaccharides
#9
Lan Yang, Juan Tang, Jin-Jun Chen, Ai-Yun Peng, Qi-Ming Wang, Li-Qun Rao, Hua Yang, Xian-Wen Zhang, Huan-Zhi Yang, Chen Zhang, Guo-Ping Peng
Poria cocos (P. cocos) polysaccharides (PCPs) are used to improve immunity and possess antitumor activities. We compared three cultivars of P. cocos (5.78, XJ 28 and JHYH) PCP contents. Then we determined that malZ, galA, SORD, gnl and bglX are key enzymes within the PCP biosynthetic pathway by using HiSeq2500 transcriptome and qRT-PCR validation. Our results provide more detailed information about the PCP biosynthesis pathway at the molecular level in P. cocos and establish the functions for the molecular breeding to produce polysaccharides in general for therapeutic use in Chinese medicinal plants...
July 16, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/30010405/cytotoxic-lanostane-triterpenoids-from-the-stems-of-schisandra-glaucescens
#10
Yan Liu, Jiang Hu, Yan Lv, Xiao-Yun Huang, Guo-Xu Zhang
Phytochemical investigation on the stems of Schisandra glaucescens resulted into the isolation of three new lanostane triterpenoids, 12-hydroxyschiglausin B (1), 12-hydroxykadsuphilactone B (2), and 20R-hydroxyschinalactone C (3). Structural elucidation of all the compounds was accomplished by spectral methods. The isolated compounds were tested in vitro for cytotoxic activities. As a result, triterpenoids 1 and 2 showed cytotoxic activities for all six tested tumor cell lines with IC50 values less than 15 μM...
July 16, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/30001634/two-new-tetracyclic-triterpenoids-from-the-endophytic-fungus-hypoxylon-sp-6269
#11
Han-Qiao Liang, Da-Wei Zhang, Shun-Xing Guo, Jie Yu
Two new tetracyclic triterpenoids, integracide E (1) and isointegracide E (2), as well as three known secondary metabolites (i.e. integracide A (3), 2-deoxyintegracide A (4) and 2-deoxyintegracide B (5)), were isolated from mycelium of the endophytic fungus Hypoxylon sp. 6269. Structures were determined by a combination of 1D and 2D NMR techniques and mass spectrometry. All of the compounds were tested for their anti-HIV-1 integrase activities.
July 12, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/29996686/anti-inflammatory-diterpenes-from-the-fruits-of-vitex-trifolia-l-var-simplicifolia-cham
#12
Shi-Ming Fang, Rui Liu, Lin Li, Jin-Long Yao, Er-Wei Liu, Guan-Wei Fan, Han Zhang, Xiu-Mei Gao
Two new labdane-type diterpenes, named viterotulin C (1) and vitexilactone D (2), together with five known diterpenes (3-7), were isolated from the fruits of Vitex trifolia L. var. simplicifolia Cham. Their structures were elucidated by detailed analysis of spectroscopic data. All the compounds were evaluated for their inhibitory effects on nuclear factor-kappa B (NF-κB) pathway in HEK 293 cell line. These compounds presented inhibition on TNF-α-induced NF-κB activation, with inhibition rates ranging from 42...
July 12, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/29996684/two-pairs-of-phenylpropanoid-enantiomers-from-the-leaves-of-eucommia-ulmoides
#13
Xu-Liu Shi, Jian-Kun Yan, Wen-Kai Li, Paul Owusu Donkor, Xiu-Mei Gao, Li-Qin Ding, Feng Qiu
Two pairs of phenylpropanoid enantiomers, (+)-(7S,8S)-alatusol D (1a), (-)-(7R,8R)-alatusol D (1b), (-)-(7S,8R)-alatusol D (2a) and (+)-(7R,8S)-alatusol D (2b) were isolated from the leaves of Eucommia ulmoides Oliver. Among them, 1a and 2b were firstly obtained by chiral enantiomeric resolution. Their structures were elucidated based on extensive spectroscopic analysis and the induced CD (ICD) spectrum caused by adding Mo2 (AcO)4 in DMSO. All compounds were tested on Hep G2 tumor cell lines. However, none of the compounds showed potential cytotoxic activity against Hep G2 in vitro...
July 12, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/29991292/synthesis-and-evaluation-of-coumarin-1-2-4-oxadiazole-hybrids-as-selective-bche-inhibitors-with-neuroprotective-activity
#14
Juan Zhang, Jia-Cheng Li, Jia-Li Song, Zhi-Qiang Cheng, Ji-Zheng Sun, Cheng-Shi Jiang
A series of new coumarin/1,2,4-oxadiazole hybrids were synthesized and evaluated for cholinesterase inhibitory and neuroprotective activities. Among them, enantiomers 5u and 5v showed potent hBChE inhibitory activity with IC50 values of 8.17 and 9.56 μM, respectively, and also exhibited good selectivity for hBChE over hAChE by 9.49- and 7.58-fold, respectively. In addition, both compounds could protect SH-SY5Y cells against Aβ25-35 -induced neurotoxicity. The preliminary bioassay results provided a new chemotype for multifunctional anti-Alzheimer's disease agents and continuing investigation into compounds 5u and 5v is warranted...
July 10, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/29989425/enzymatic-synthesis-of-glucuronidated-metabolites-of-two-neurological-active-agents-using-plant-glucuronosyltransferases
#15
Tian Yue, Ke-Bo Xie, Zhen Tan, Ri-Dao Chen, Da-Wei Chen, Ji-Mei Liu, Jun-Gui Dai
Glucuronidation is an important and popular metabolic reaction in vivo of drugs. The further evaluation of biological activity and toxicity of glucuronides is necessary in the course of the drug research and development. However, the synthesis of glucuronides is limited by the lack of efficient approach. Herein, we have developed a new glucuronide synthesis method using plant uridine diphosphate-dependent glucuronosyltransferases (UGTs), UGT88D4, UGT88D7, and EpGT8, enabling the convenient preparation for corresponding O-glucuronide metabolites (1a, 2a, 3a, and 3b) in milligram scale of two neurological active agents, IMM-H004 (1) and FLZ (2)...
July 10, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/29986612/nimbandiolactone-21-and-nimbandioloxyfuran-two-new-28-norlimonoids-from-the-leaves-of-azadirachta-indica-meliaceae
#16
Nhi Y Thi Nguyen, Phu Hoang Dang, Van Truong Thien Nguyen, Tuan Trong Vo, Dao Anh Thi Nguyen, Minh Duc Huu Nguyen, Phuc Huu Dang, Quan Le Tran
From an EtOAc-soluble fraction of the leaves of Azadirachta indica, two new 28-norlimonoids named nimbandiolactone-21 (1) and nimbandioloxyfuran (2), together with nimbandiolactone-23 (3), were isolated. Their relative structures were elucidated based on NMR spectroscopic interpretation and biosynthetic consideration. Nimbandioloxyfuran (2) and nimbandiolactone-23 (3) showed potent α-glucosidase inhibitory activity, with the IC50 values of 46.2 and 38.7 μM, respectively.
July 9, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/29985069/-%C3%A2-cochlearoids-n-p-three-pairs-of-phenolic-meroterpenoids-from-the-fungus-ganoderma-cochlear-and-their-bioactivities
#17
Fu-Ying Qin, Yong-Ming Yan, Zheng-Chao Tu, Yong-Xian Cheng
Three pairs of meroterpenoids (±) cochlearoids N-P (1-3) were isolated from the fruiting bodies of Ganoderma cochlear. Their structures including absolute configurations were assigned by spectroscopic techniques. All the isolated compounds were tested for their inhibitory activities toward BRD4, human cancer cells, and micro-organisms. The results show that the enantiomers of (±)-1 are BRD4 inhibitors, (-)-1 and (+)-3 are cytotoxic against human cancer cells (K562) with IC50 values of 7.68 and 6.68 μM, respectively...
July 9, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/29974799/stereoselective-synthesis-of-4%C3%AE-acyloxypodophyllotoxin-derivatives-as-insecticidal-agents
#18
Zhi-Ping Che, Yue-E Tian, Sheng-Ming Liu, Jia Jiang, Mei Hu, Gen-Qiang Chen
As our ongoing work on research of natural-product-based insecticidal agents, some 4α/β-acyloxypodophyllotoxin derivatives were synthesized, and were evaluated against the pre-third-instar larvae of B. mori, A. dissimilis and M. separate in vivo at the concentration of 1 mg ml-1 , respectively. Among all derivatives, compounds 2 g, h and 4c, d showed more promising insecticidal activities than their precursors - podophyllotoxin and epipodophyllotoxin. Furthermore, derivatives 2 g, h and 4c, d exhibited more relative amicable activities than their precursors - podophyllotoxin and epipodophyllotoxin...
July 5, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/29973097/eupatilin-a-natural-pharmacologically-active-flavone-compound-with-its-wide-range-applications
#19
Bushra Nageen, Iqra Sarfraz, Azhar Rasul, Ghulam Hussain, Fariha Rukhsar, Somia Irshad, Ammara Riaz, Zeliha Selamoglu, Muhammad Ali
Eupatilin (5,7-dihydroxy-3',4',6-trimethoxyflavone) is a pharmacologically active flavone which has been isolated from a variety of medicinal plants. Eupatilin is known to possess various pharmacological properties such as anti-cancer, anti-oxidant, and anti-inflammatory. It is speculated that eupatilin could be subjected to structural optimization for the synthesis of derivative analogs to reinforce its efficacy, to minimize toxicity, and to optimize absorption profiles, which will ultimately lead towards potent drug candidates...
July 4, 2018: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/29972031/a-new-flavonoid-derivative-and-a-new-5-hydroxyanthranilic-acid-derivative-from-the-sea-urchin-derived-streptomyces-sp-hda1
#20
Zhi-Kai Guo, Rong Wang, Tian-Mi Liu, Fu-Xiao Chen, Ming-Qiu Yang
One new flavonoid derivative flavoside A (1), one new 5-hydroxyanthranilic acid derivative crassilin (2), along with the known angucyclinone PD116740 (3) and oxachelin (4), was isolated from the EtOAc extract of the fermentation broth of the sea urchin (Anthocidaris crassispina)-derived actinobacterium, Streptomyces sp. HD01. The structures of these compounds were established on the basis of their HR-ESI-MS and NMR spectroscopic data. All of these compounds were assessed for their antibacterial activity.
July 4, 2018: Journal of Asian Natural Products Research
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